Graphene oxide as a nanocarrier for controlled release and targeted delivery of an anticancer active agent, chlorogenic acid

Mater Sci Eng C Mater Biol Appl. 2017 May 1:74:177-185. doi: 10.1016/j.msec.2016.11.114. Epub 2016 Dec 5.

Abstract

We have synthesized graphene oxide using improved Hummer's method in order to explore the potential use of the resulting graphene oxide as a nanocarrier for an active anticancer agent, chlorogenic acid (CA). The synthesized graphene oxide and chlorogenic acid-graphene oxide nanocomposite (CAGO) were characterized using Fourier transform infrared (FTIR) spectroscopy, thermogravimetry and differential thermogravimetry analysis, Raman spectroscopy, powder X-ray diffraction (PXRD), UV-vis spectroscopy and high resolution transmission electron microscopy (HRTEM) techniques. The successful conjugation of chlorogenic acid onto graphene oxide through hydrogen bonding and π-π interaction was confirmed by Raman spectroscopy, FTIR analysis and X-ray diffraction patterns. The loading of CA in the nanohybrid was estimated to be around 13.1% by UV-vis spectroscopy. The release profiles showed favourable, sustained and pH-dependent release of CA from CAGO nanocomposite and conformed well to the pseudo-second order kinetic model. Furthermore, the designed anticancer nanohybrid was thermally more stable than its counterpart. The in vitro cytotoxicity results revealed insignificant toxicity effect towards normal cell line, with a viability of >80% even at higher concentration of 50μg/mL. Contrarily, CAGO nanocomposite revealed enhanced toxic effect towards evaluated cancer cell lines (HepG2 human liver hepatocellular carcinoma cell line, A549 human lung adenocarcinoma epithelial cell line, and HeLa human cervical cancer cell line) compared to its free form.

Keywords: Anticancer property; Drug delivery; Graphene oxide; Nanocomposite; Sustained release.

MeSH terms

  • A549 Cells
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / toxicity
  • Cell Survival / drug effects
  • Chlorogenic Acid / chemistry*
  • Chlorogenic Acid / toxicity
  • Delayed-Action Preparations / chemistry
  • Drug Liberation
  • Graphite / chemistry*
  • HeLa Cells
  • Hep G2 Cells
  • Humans
  • Hydrogen Bonding
  • Hydrogen-Ion Concentration
  • Microscopy, Electron, Transmission
  • Nanocomposites / chemistry*
  • Oxides / chemistry
  • Spectroscopy, Fourier Transform Infrared
  • Spectrum Analysis, Raman
  • Thermogravimetry
  • X-Ray Diffraction

Substances

  • Antineoplastic Agents
  • Delayed-Action Preparations
  • Oxides
  • Chlorogenic Acid
  • Graphite